Field of Invention
The disclosure relates to a pharmaceutical formulation. More particularly, the disclosure relates to a pharmaceutical formulation containing glycosaminoglycan.
Description of Related Art
Enteric coating has been developed for many years to improve the treatment efficiency of enteric diseases, and the used dose of drug can be thus decreased. However, the treatment efficiency of enteric diseases still needs improvement to further decrease the used dose of drug.
Mesalamine, also known as Mesalazine or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammation of the digestive tract ulcerative colitis and mild-to-moderate Crohn's disease. Mesalamine is a bowel-specific aminosalicylate drug that acts locally in the gut and has its predominant actions there, thereby having few systemic side effects. As a derivative of salicylic acid, mesalamine is also thought to be an antioxidant that traps free radicals, which are potentially damaging byproducts of metabolism. N-acetyl-5-ASA is a metabolite of 5-ASA. The absorbed 5-ASA is rapidly acetylated through the gut mucosal wall and by the liver. It is mainly excreted by the kidney, as N-acetyl-5-ASA.
U.S. Pat. No. 4,980,173 discloses a pharmaceutical composition containing as active ingredient 5-aminosalicylic acid or a pharmaceutically acceptable salt or ester thereof allow the treatment of colitis ulcerosa or Crohn's disease by oral administration. A particular slow-release tablet formation and its preparation were disclosed. The defect of the patent is that the drug distributes naturally in the intestine and dispersed not specific in interesting site, so it needs more dose to achieve better therapy result and will have less therapy effect owing to less dose of the drug adhered onto the inflammation part.
U.S. Pat. No. 5,541,170 discloses a solid dosage form, such as a capsule or tablet, containing a pharmacologically active agent is coated with an anionic polymer, which is insoluble in gastric juice and in intestinal juice below pH 7 but soluble in colonic intestinal juice, in a sufficient amount that the oral dosage form remains intact until it reaches the colon. Although this invention has specifically released the drug in the environment below pH 7, it still cannot aim the target to enhance the concentration of the drug on the disorder part. The defect is all the same as aforementioned.
U.S. Pat. No. 5,541,171 also discloses a solid dosage form that so much like U.S. Pat. No. 5,541,170. This patent just added more restriction terms comparing with the former one.
U.S. Pat. No. 6,551,620 discloses an orally administerable pharmaceutical pellet formulation for the treatment of the intestinal tract that is disclosed, which comprises a core and an enteric coating, the core including, as a pharmaceutical active compound, aminosalicylic acid or a pharmaceutically tolerable salt or a derivative thereof. The defect is still all the same as aforementioned.
U.S. Pat. No. 6,773,720 discloses a controlled-release oral pharmaceutical composition containing an active ingredient 5-amino-salicylic acid. The composition comprises: (a) an inner lipophilic matrix consisting of substances with a melting point below 90° C. in which the active ingredient is at least partly inglobated; (b) an outer hydrophilic matrix in which the lipophilic matrix is dispersed; and (c) optionally other excipients. The defect is still all the same as aforementioned.
U.S. Pat. No. 6,893,662 discloses a pharmaceutical composition in a solid unit dosage form for oral administration in a human or lower animal. The pharmaceutical composition comprises: (a) a safe and effective amount of a therapeutically active agent; (b) an inner coating layer selected from the group consisting of poly(methacrylic acid, methyl methacrylate) 1:2, poly(methacrylic acid, methyl methacrylate) 1:1, and mixtures thereof; and (c) an outer coating layer comprising an enteric polymer or film coating material. However, the defect is still all the same as aforementioned.
U.S. Pat. No. 6,046,179 discloses a composition for treating inflammatory bowel disease in a patient suffering from inflammatory bowel disease comprising: (a) a therapeutic amount of N-acetyl-glucosamine; and (b) a pharmacologically acceptable carrier, adapted to be administered colonically to said patient. The defect of this patent is that it was short of a drug other than N-acetyl-glucosamine; therefore, it lacks supplement each other between N-acetyl-glucosamine and the other drug, such as mesalamine.
Since the compositions of these patents above all have to be used under regular doses of either drug or N-acetyl-glucosamine, these compositions cannot decrease the general therapeutic dose (amount) of either one.
Glycosaminoglycan can be obtained from numerous sources (e.g. rooster combs, trachea, umbilical cords, skin, articular fluids and certain bacteria such as Streptococci spp). Most glycosaminoglycans are composed of repeating sugars such as N-acetyl glucosamine, N-acetyl glucuronic acid and/or N-acetyl galactosamine (these are known as non-sulfated glycosaminoglycans). If such glycosaminoglycans contain sulfur groups they are known as sulfated glycosaminoglycans. Examples of glycosaminoglycans include hyaluronic acid (which is made up of repeating units of N-acetyl glucosamine and glucuronic acid), chondroitin sulphate, dermatan sulphate, keratan sulphate and heparin, all of which contain either N-acetylglucosamine or the amino sugar, N-acetylgalactosamine. Glycosaminoglycans are also presented in proteoglycans, which are structures containing a number of glycosaminoglycans chains linked to a polypeptide or a protein core.